Person: TÜRE, ASLI
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TÜRE
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ASLI
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Publication Metadata only Novel fluoroquinolones containing 2-arylamino-2-oxoethyl fragment: Design, synthesis, evaluation of antibacterial and antituberculosis activities and molecular modeling studies(WILEY, 2022) TÜRE, ASLI; Kulabas, Necla; Ture, Asli; Bozdeveci, Arif; Krishna, Vagolu Siva; Karaoglu, Sengul Alpay; Sriram, Dharmarajan; Kucukguzel, IlkayNovel substituted fluoroquinolone derivatives, compounds 6-20 were designed, synthesized, and evaluated for antituberculosis and antibacterial activity. Antibacterial activities of the compounds were determined and compound 14 was found to be the most potent antimicrobial agent owing to minimal inhibitory concentration (MIC) value of <1.16 mu g/mu l for all tested bacteria. Further, compounds were tested in vitro for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Most of the compounds showed antimycobacterial effects with 1.56-25.00 mu g/ml MIC values. Compounds 14 and 18 were found to be the most active derivatives due to their MIC at 1.56 mu g/ml. Selected compounds 11, 14, 17, and 18 were tested for M. tuberculosis DNA supercoiling assay and they had IC50 values within a range of 6.35-15 mu M. Mechanism of binding to DNA gyrase enzymes was evaluated using in silico molecular modeling studies and it was shown that compounds 6-20 adopt a similar binding mode as already known for fluoroquinolone drugs.Publication Metadata only Design, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2019) TÜRE, ASLI; Ture, Asli; Kulabas, Necla; Dingis, Serap Ipek; Birgul, Kaan; Bozdeveci, Arif; Karaoglu, Sengul Alpay; Krishna, Vagolu Siva; Sriram, Dharmarajan; Kucukguzel, IlkayTwenty-one novel alkyl/acyl/sulfonyl substituted fluoroquinolone derivatives were designed, synthesized and evaluated for their anti-tuberculosis and antibacterial activity. The targeted compounds were synthesized by the introduction of alkyl, acyl or sulfonyl moieties to the basic secondary amine moiety of moxifloxacin. Structures of the compounds were enlightened by FT-IR, H-1 NMR, C-13 NMR and HRMS data besides elemental analysis. Compounds were initially tested in vitro for their anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv using microplate alamar blue assay. Minimal inhibitory concentration (MIC) values of all compounds were found between > 25.00-0.39 mu g/mL while compounds 1, 2 and 13 revealed an outstanding activity against M. tuberculosis H37Rv with MIC values of 0.39 mu g/mL. Activities of compounds 1-21 against to a number of Gram-positive and Gram-negative bacteria and fast growing mycobacterium strain were also investigated by agar well diffusion and microdilution methods. According to antimicrobial activity results, compound 13 was found the most potent derivative with a IC50 value of < 1.23 mu g/mL against Staphylococcus aureus and clinical strain of methicillin-resistant clinical strain of S. aureus.